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  1. General Info
  2. Source Info
  3. Effects Info
  4. Reference
Phytochemical Details
01. General Information
Name Costunolide
PubChem CID 5281437
Molecular Weight 232.32g/mol
Synonyms

costunolide, isocostunolide

Formula C₁₅H₂₀O₂
SMILES CC1=CCCC(=CC2C(CC1)C(=C)C(=O)O2)C
InChI 1S/C15H20O2/c1-10-5-4-6-11(2)9-14-13(8-7-10)12(3)15(16)17-14/h5,9,13-14H,3-4,6-8H2,1-2H3/b10-5+,11-9+/t13-,14+/m0/s1
InChIKey HRYLQFBHBWLLLL-AHNJNIBGSA-N
CAS Number 553-21-9
ChEMBL ID CHEMBL86416
ChEBI ID CHEBI:3900
Herb ID HBIN021599
KEGG ID C09382
Structure 2D-img
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2D MOL 3D MOL
02. Source Information of Phytochemical
(1) Dolomiaea souliei Warm
Chineses Pinyin ChuanMuXiang
Use Part Root
Habitat SiChuan, XiZang
Flavor Pungent, Bitter
Meridian Tropism Spleen, Stomach, Large intestine, Gallbladder
Species
>Kingdom: Viridiplantae
 -->Phylum: Streptophyta
  -->Class: Equisetopsida
   -->Order: Asterales
    -->Family: Asteraceae
     -->Genus: Dolomiaea
      -->Species: Dolomiaea souliei
(2) Aucklandia lappa Warm
Chineses Pinyin MuXiang
Use Part Root
Habitat YunNan, SiChuan
Flavor Pungent, Bitter
Meridian Tropism Spleen, Stomach, Large intestine, Triple burner, Gallbladder
Species
>Kingdom: Viridiplantae
 -->Phylum: Streptophyta
  -->Class: Equisetopsida
   -->Order: Asterales
    -->Family: Asteraceae
     -->Genus: Aucklandia
      -->Species: Aucklandia lappa
(3) Momordica cochinchinen-sis Cold
Chineses Pinyin MuBieGen
Use Part Tuberoid
Habitat JiangSu, AnHui, JiangXi, FuJian, TaiWan, GuangDong, GuangXi, HuNan, SiChuan, GuiZhou
Flavor Bitter, Mildly sweet
(4) Laurus nobilis Warm
Chineses Pinyin YueGuiYe
Use Part Leaf
Habitat JiangSu, ZheJiang, FuJian, TaiWan, SiChuan, YunNan
Flavor Pungent
Species
>Kingdom: Viridiplantae
 -->Phylum: Streptophyta
  -->Class: Equisetopsida
   -->Order: Laurales
    -->Family: Lauraceae
     -->Genus: Laurus
      -->Species: Laurus nobilis
(5) Saussurea costus Warm
Chineses Pinyin YunMuXiang
Use Part Root
Flavor Pungent; Bitter
Meridian Tropism Spleen; Stomach; Large intestine; Gallbladder; Triple Energizers
Species
>Kingdom: Viridiplantae
 -->Phylum: Streptophyta
  -->Class: Magnoliopsida
   -->Order: Asterales
    -->Family: Asteraceae
     -->Genus: Saussurea
      -->Species: Saussurea costus
03. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Drug(s) whose efficacy can be enhanced by this phytochemical
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Combination Pair ID: 231
Pair Name Costunolide, Doxorubicin
Partner Name Doxorubicin
Disease Info [ICD-11: 2C82] Prostate cancer Investigative
Biological Phenomena Induction-->ROS generation
Gene Regulation Up-regulation Phosphorylation MAPK14 hsa1432
Up-regulation Phosphorylation MAPK8 hsa5599
Up-regulation Expression ROS1 hsa6098
In Vitro Model DU145 Prostate carcinoma Homo sapiens (Human) CVCL_0105
PC-3 Prostate carcinoma Homo sapiens (Human) CVCL_0035
In Vivo Model PC-3 cells (3×10⁶) were injected subcutaneously into the armpit of each mouse.
Result We suggested that costunolide in combination with doxorubicin was a new potential chemotherapeutic strategy for treating prostate cancer.
Combination Pair ID: 705
Pair Name Costunolide, Imatinib
Partner Name Imatinib
Disease Info [ICD-11: 2B33.3] Acute lymphoblastic leukemia Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Up-regulation Cleavage CASP3 hsa836
In Vitro Model K-562 Blast phase chronic myelogenous leukemia Homo sapiens (Human) CVCL_0004
Result These results demonstrate that costunolide may be a potent therapeutic agent against chronic myeloid leukemia.
Combination Pair ID: 706
Pair Name Costunolide, Doxorubicin
Partner Name Doxorubicin
Disease Info [ICD-11: 2B33.3] Acute lymphoblastic leukemia Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Down-regulation Phosphorylation AKT1 hsa207
Up-regulation Cleavage CASP3 hsa836
Down-regulation Phosphorylation PIK3CA hsa5290
In Vitro Model K-562 Blast phase chronic myelogenous leukemia Homo sapiens (Human) CVCL_0004
Result These results demonstrate that costunolide may be a potent therapeutic agent against chronic myeloid leukemia.
Combination Pair ID: 1040
Pair Name Costunolide, Osimertinib
Partner Name Osimertinib
Disease Info [ICD-11: 2C25] Lung cancer Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Down-regulation Phosphorylation AKT1 hsa207
Down-regulation Phosphorylation GSK3B hsa2932
Down-regulation Phosphorylation MAP2K1 KEGG ID N.A.
Down-regulation Phosphorylation MAPK1 hsa5594
Down-regulation Phosphorylation NFKB1 hsa4790
Down-regulation Phosphorylation RPS6KA3 KEGG ID N.A.
In Vitro Model PC-9 Lung adenocarcinoma Homo sapiens (Human) CVCL_B260
HCC827 Lung adenocarcinoma Homo sapiens (Human) CVCL_2063
NCI-H1975 Lung adenocarcinoma Homo sapiens (Human) CVCL_1511
In Vivo Model 6–7 weeks old female mice with severe combined immunodeficiency (SCID) were employed to eatablish osimertinib-resistant PDX model.
Result The combination of osimertinib and costunolide showed synergistic or additive inhibitory effects on tumor growth in osimertinib-resistant cell lines and PDX model. Hence, this study highlights a potential therapeutic strategy for osimertinib-resistant patients through targeting of MEK1 and AKT1/2 by costunolide.
04. Reference
No. Title Href
1 Costunolide enhances doxorubicin-induced apoptosis in prostate cancer cells via activated mitogen-activated protein kinases and generation of reactive oxygen species. Oncotarget. 2017 Nov 21;8(64):107701-107715. doi: 10.18632/oncotarget.22592. Click
2 Costunolide promotes imatinib-induced apoptosis in chronic myeloid leukemia cells via the Bcr/Abl-Stat5 pathway. Phytother Res. 2018 Sep;32(9):1764-1769. doi: 10.1002/ptr.6106. Click
3 Costunolide enhances sensitivity of K562/ADR chronic myeloid leukemia cells to doxorubicin through PI3K/Akt pathway. Phytother Res. 2019 Jun;33(6):1683-1688. doi: 10.1002/ptr.6355. Click
4 Costunolide is a dual inhibitor of MEK1 and AKT1/2 that overcomes osimertinib resistance in lung cancer. Mol Cancer. 2022;21(1):193. Published 2022 Oct 6. doi:10.1186/s12943-022-01662-1 Click
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